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Jatrorrhizine

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Chemical Structure| 3621-38-3 同义名 : Neprotin;Yatrorizine
CAS号 : 3621-38-3
货号 : A840009
分子式 : C20H20NO4
纯度 : 99%+
分子量 : 338.38
MDL号 : MFCD01310242
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 3 mg/mL(8.87 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 5 mg/mL(14.78 mM),配合低频超声助溶

动物实验配方:
生物活性
靶点
  • AChE

    AChE, IC50:872 nM

描述 Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective. In vitro uptake tests showed that jatrorrhizine strongly inhibited PMAT-mediated MPP+ uptake with an IC50 value of 1.05 μM and reduced 5-HT and NE uptake mediated by hOCT2, hOCT3 and hPMAT with IC50 values of 0.1-1 μM (for OCT2 and OCT3) and 1-10 μM (for PMAT)[3]. Moreover, jatrorrhizine distinctly inhibited the proliferation of MDA-MB-231, MCF-7 and 4T1 cells with IC50 values of 11.08 ± 1.19 μM, 17.11 ± 4.54 μM and 22.14 ± 2.87 μM, induced mitochondrial dysfunction and early apoptosis involving mitochondrial apoptotic pathway[4]. JAT (Jatrorrhizine) inhibited the proliferation of HCT-116 and HT-29 cells with IC50 values of 6.75±0.29 μM and 5.29±0.13 μM, respectively, for 72 hrs. In addition, JAT inhibited Wnt signaling pathway by reducing β-catenin and increasing GSK-3β expressions. In HCT-116 nude mice xenograft model, JAT inhibited tumor growth and metastasis, and induced apoptosis of tumor cells[5]. Jatrorrhizine dose-dependently (0.1, 0.3 and 1 mg/kg) offset delayed gastric emptying and intestinal transit (geometric centre and the migration of Evans blue) in postoperative ileus[6]. JAT administration could alleviate the learning and memory deficits in AD. Furthermore, JAT treatment reduced the levels of Aβ plaques in the cortex and hippocampus of APP/PS1 double-transgenic mice[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.78mL

2.96mL

1.48mL

29.55mL

5.91mL

2.96mL

参考文献

[1]Wu H, He K, et al. The antihypercholesterolemic effect of jatrorrhizine isolated from Rhizoma Coptidis. Phytomedicine. 2014 Sep 25;21(11):1373-81.

[2]Li J, Li J, et al. Spectroscopic analysis and molecular modeling on the interaction of jatrorrhizine with human serum albumin (HSA). Spectrochim Acta A Mol Biomol Spectrosc. 2014 Jan 24;118:48-54.

[3]Sun S, Zhou S, Lei S, Zhu S, Wang K, Jiang H, Zhou H. Jatrorrhizine reduces 5-HT and NE uptake via inhibition of uptake-2 transporters and produces antidepressant-like action in mice. Xenobiotica. 2019 Oct;49(10):1237-1243

[4]Sun Y, Gao X, Wu P, Wink M, Li J, Dian L, Liang Z. Jatrorrhizine inhibits mammary carcinoma cells by targeting TNIK mediated Wnt/β-catenin signalling and epithelial-mesenchymal transition (EMT). Phytomedicine. 2019 Oct;63:153015

[5]Wang P, Gao XY, Yang SQ, Sun ZX, Dian LL, Qasim M, Phyo AT, Liang ZS, Sun YF. Jatrorrhizine inhibits colorectal carcinoma proliferation and metastasis through Wnt/β-catenin signaling pathway and epithelial-mesenchymal transition. Drug Des Devel Ther. 2019 Jul 8;13:2235-2247

[6]Zhang B, Cao A, Zhou J, Hu Z, Wu D. Effect of jatrorrhizine on delayed gastrointestinal transit in rat postoperative ileus. J Pharm Pharmacol. 2012 Mar;64(3):413-9

[7]Wang S, Jiang W, Ouyang T, Shen XY, Wang F, Qu YH, Zhang M, Luo T, Wang HQ. Jatrorrhizine Balances the Gut Microbiota and Reverses Learning and Memory Deficits in APP/PS1 transgenic mice. Sci Rep. 2019 Dec 20;9(1):19575